LSD1-IN-14

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LSD1-IN-14 

LSD1-IN-14 是一种有效且具有选择性的 LSD1 抑制剂 (IC50=0.89 μM)。LSD1-IN-14 能显著抑制 A549 和 THP-1 细胞的增殖，能诱导肿瘤细胞的凋亡。

LSD1-IN-14

LSD1-IN-14 Chemical Structure

CAS No. : 2698340-11-1

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生物活性

LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells[1].

IC50 & Target

IC50: 0.89 μM (LSD1)[1]
体外研究
(In Vitro)

LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively[1].
LSD1-IN-14 (0-3 μM ;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner[1].
LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner[1].
LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T1/2 of 103.3 min and Clint(mic) of 13.4 μL/min/mg[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: A549 and THP-1[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively.

Western Blot Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.3, 1 and 3 μM
Incubation Time: 72 hours
Result: Significantly upregulated the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner.

Apoptosis Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.3, 1 and 3 μM
Incubation Time: 72 hours
Result: Induced the apoptosis of 53.6% of cells in a dose-dependent manner.

体内研究
(In Vivo)

LSD1-IN-14 (2 mg/kg for i.v., 10 mg/kg for i.g, single) has an acceptable half-life and oral bioavailability[1].
Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1].

IV (2 mg/kg) IG (10 mg/kg)
C0 (ng/mL) 575 Cmax (ng/mL) 41.1
T1/2 (h) 1.0 T1/2 (h) 2.8
Vdss (L/kg) 6.6 Tmax (h) 0.8
Cl (mL/min/kg) 156 AUC0-t (ng.h/mL) 126
AUC0-t (ng.h/mL) 211 AUC0-∞ (ng.h/mL) 152
AUC0-∞ (ng.h/mL) 214 Bioacailability (%) 11.9

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 2 mg/kg for i.v., 10 mg/kg for i.g.
Administration: i.v. and i.g, single
Result: Showed an acceptable half-life and oral bioavailability.

分子量

365.45

Formula

C21H24FN5
CAS 号

2698340-11-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wang X, et al. Design, synthesis and biological evaluation of 2-aminopyrimidine-based LSD1 inhibitors. Bioorg Chem. 2022;121:105699.

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